Development and In-Vivo Evaluation of Buccal Tablets Prepared Using Danazol-Sulfobutylether 7 β-Cyclodextrin (SBE 7) Complexes

摘要

The aim of the present work was to develop a mucoadhesive controlled release formulation of danazol-SBE 7 β-CD complex and to evaluate the feasibility of improving the bioavailability of danazol via the buccal route. Different types of polymers, Polycarbophil (PC) and HPMC were mixed with danazol-SBE 7 complex and compressed into tablets. In vivo bioavailability performed in dogs showed that the perorally administered danazol-SBE 7 complex and the danazol-SBE 7 (in PC matrix) buccal tablets had absolute bioavailabilities of 64% and 25% respectively, that were significantly greater than 1.8% observed for the commercial formulation Danocrine~(~R). The increased bioavailability was due to the enhanced solubility consequent to complexation, and the possible avoidance of first-pass metabolism upon buccal administration.